Table 3.
Permeability results (Pe, 10−6 cm/s) from the PAMPA–BBB assay for compounds 12, 20–24, 30–38, and 52 and their prediction of BBB penetration.
| Compd. | Pe (10−6 cm/s)a | Predictionb |
|---|---|---|
| NTZ | 1.26±0.21 | CNS+/− |
| 12 | 5.76±0.57 | CNS+ |
| 20 | 0.45±0.03 | CNS− |
| 21 | 0.09±0.01 | CNS− |
| 22 | 6.02±0.27 | CNS+ |
| 23 | 4.92±0.31 | CNS+ |
| 24 | 12.62±1.22 | CNS+ |
| 30 | 5.76±0.55 | CNS+ |
| 31 | 3.42±0.07 | CNS+ |
| 32 | 6.16±0.50 | CNS+ |
| 33 | 10.41±1.25 | CNS+ |
| 34 | 6.82±0.50 | CNS+ |
| 35 | 9.24±0.47 | CNS+ |
| 36 | 10.62±0.10 | CNS+ |
| 37 | 9.89±0.37 | CNS+ |
| 38 | 9.88±0.75 | CNS+ |
| 52 | 10.50±1.13 | CNS+ |
Values are expressed as the mean ± SD (n ≥ 3).
Compounds with permeabilities Pe > 3.08 × 10−6 cm/s could cross the BBB by passive diffusion (CNS+). Compounds with Pe < 1.13 × 10−6 cm/s show low BBB permeation (CNS−), and compounds with 1.13 × 10−6 cm/s < Pe < 3.08 × 10−6 cm/s show uncertain BBB permeation (CNS+/−).